Synthesis and biological evaluation of novel hybrids of highly potent and selective α4β2-Nicotinic acetylcholine receptor (nAChR) partial agonists
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- 作者：Han-Kun Zhanga ; b ; J. Brek Eatonc ; Allison Fedolakd ; Hendra Gunosewoyoa ; 1 ; Oluseye K. Onajolea ; Dani Brunnerd ; Ronald J. Lukasc ; Li-Fang Yua ; e ; lfyu@sat.ecnu.edu.cn" class="auth_mail" title="E-mail the corresponding author ; Alan P. Kozikowskia ; kozikowa@uic.edu" class="auth_mail" title="E-mail the corresponding author
- 关键词：α4β2-nAChRs ; Partial agonists ; Hybrids ; Antidepressant-like effects
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：29 November 2016
- 年：2016
- 卷：124
- 期：Complete
- 页码：689-697
- 全文大小：767 K
文摘
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Seven novel hybrid compounds were rational designed and synthesized.
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All compounds were found to be potent and selective α4β2-nAChR binders.
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Compounds 21, 25, and 30 maintained the functional profiles of the parent compounds.
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In vivo efficacy of compound 21 was confirmed in SmartCube® and forced swim tests.